Patent SG-11201804594Y-A (SG)
Title: L-valinate of hydroxypropylthiazolidine carboxamide derivative and salt form, crystal polymorph thereof
Inventor: NAXOS PAGE PATRICK
IPC: C07D277/06
Filed: 2017-01-04
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property -' Organization International Bureau res:0) (43) International Publication Date .... ....r .....) 13 July 2017 (13.07.2017) WI P0 I P CT (10) WO International 1111111111113111111111111111111111111111111111111111111111111111111111111111111111111111 2017/118641 Publication Number Al (51) International Patent Classification: SCHWARZ, Matthias; 43, Rue Philippe Plantamour, C07D 277/06 (2006.01) A61P 15/00 (2006.01) 1201 GenOve (CH). JORAND-LEBRUN, Catherine; A61K 31/426 (2006.01) A61P 15/06 (2006.01) Chef Lieu, 74270 Contamine-Sarzin (FR). QUATTRO- A61K 45/06 (2006.01) PANI, Anna; Rte de Cherie 2, 1207 GenOve (CH). POMEL, Vincent; 228, Chemin du Bois des Presses, (21) International Application Number: PCT/EP2017/050101 74570 Groisy (FR). (74) Agent: KATZAROV S.A.; 19 rue des Epinettes, 1227 (22) International Filing Date: GenOve (CH). 4 January 2017 (04.01.2017) (25) Filing Language: English (81) Designated States (unless otherwise indicated, for every kind of national protection available): AE, AG, AL, AM, (26) Publication Language: English AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, (30) Priority Data: DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, 14/987,586 4 January 2016 (04.01.2016) US HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, ICH, KN, 62/274,674 4 January 2016 (04.01.2016) US KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, 62/395,664 16 September 2016 (16.09.2016) US MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, 62/407,918 13 October 2016 (13.10.2016) US NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, (71) Applicant: MERCK SERONO S.A. [CH/CH]; Centre In- RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, dustriel, 1267 Coinsins (CH). TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (72) Inventors: NAXOS PAGE, Patrick; Les Cyclades, Aven- ue de GenOve, 74160 Saint-Julien-en-Genevois (CH). [Continued on next page] (54) Title: L-VALINATE OF HYDROXYPROPYLTHIAZOLIDINE CARBOXAMIDE DERIVATIVE AND SALT FORM, CRYSTAL POLYMORPH THEREOF (57) : The invention the L- provides valinate ester of a hydroxypropylthiazolidine ( I) F derivative formula carboxamide of (I), (2S)- 3-([1,1'-biphenyl]-4-ylsulfony1)-N-[(1S)-3- hydroxy-1- phenylpropy1]-1,3-thiazolidine-2- 0 carboxamide, as well as salts and crystal cA , poly- ip...Nh, s sm morphs thereof. The compound inhibits the ‘\") 4 11 F receptor (PGF2alpha) and is a prostaglandin useful the treatment of such as Irl in disorders preterm labor at the early gestational stage or FIG. 1 dysmennorrhea. 4 -.:-.c.-,=.:.= Il .4t Il - P-- W - .4 Gni - veins)) -- 4\" - Atzwianat i t 4 Ott - $siR$tit4 . , 1 3 3 tan x initash, rn Il it--- , pel i'M lz ves4de-rckinf& p.m 11 C ei O WO 2017/118641 Al MMEDIMOMOIDEIRMEM3011111011001VOIRVOIS (84) Designated States (unless otherwise indicated, for every SI, SK, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, kind of regional protection available): ARIPO (BW, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, GH, SZ, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, Published: RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, CZ, IT, RS, DE, — LT, SE, with international search report (Art. 21(3))